The present application relates to crystalline forms of lifitegrast that are useful for the development and optimization of a pharmaceutical composition containing lifitegrast.
The chemical name for lifitegrast is (S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid. The molecular formula of lifitegrast is C29H24C12N2O7S and its molecular weight is 615.5. The strucgtural formula of lifitegrast is:

Xiidra (lifitegrast ophthalmic solution) 5% is a lymphocyte function-associated antigen-1 (LFA-1) antagonist indicated for the treatment of the signs and symptoms of dry eye disease (DED).
U.S. Pat. No. 8,367,701B2 and U.S. Patent Application Publication No. 2015/0336939A1 disclose six crystalline forms of lifitegrast. These crystalline forms have their inevitable shortcoming. For example, these crystalline forms are not easy to prepare.
Therefore, there remains a need for the development of improved form of lifitegras.